MLN8054
Based on 10 publication(s) in Google Scholar
MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.01%
- No. CAS: 869363-13-3
- Fòrmula: C25H15ClF2N4O2
- Peso molecular:476.86
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) MLN8054
More- Cancer Res. 2017 Sep 15;77(18):4785-4796. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- PLoS Biol. 2020 Jun 9;18(6):e3000288. [Abstract]
- EMBO Rep. 2021 Jul 5;22(7):e51847. [Abstract]
- Comput Struct Biotechnol J. 2019 Feb 8:17:352-361. [Abstract]
- Mol Cell Endocrinol. 2025 Aug 28:609:112645. [Abstract]
- Anticancer Drugs. 2024 Jan 1;35(1):46-54. [Abstract]
- Patent. US20210299273A1.
- Technical University of Munich. 24.01.2018.
- J Biomol Screen. 2013 Oct;18(9):1062-71. [Abstract]
Ver todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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Aurora A 4 nM (IC50) |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Calu-6 | IC50 |
0.22 μM
Compound: MLN-8054
|
Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| DLD-1 | IC50 |
1.43 μM
Compound: MLN-8054
|
Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| HCT-116 | GI50 |
0.22 μM
Compound: 8, MLN8054
|
Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay
Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay
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[PMID: 26101564] |
| HCT-116 | IC50 |
0.1 μM
Compound: 1, MLN-8054
|
Antiproliferative activity against human HCT116 cells after 4 days by celltiter assay
Antiproliferative activity against human HCT116 cells after 4 days by celltiter assay
|
[PMID: 19402633] |
| HCT-116 | IC50 |
0.16 μM
Compound: 1, MLN-8054
|
Inhibition of Aurora A in human HCT116 cells assessed as complete failure of centrosome seperation by immunofluorescence assay
Inhibition of Aurora A in human HCT116 cells assessed as complete failure of centrosome seperation by immunofluorescence assay
|
[PMID: 19402633] |
| HCT-116 | IC50 |
0.18 μM
Compound: MLN-8054
|
Antiproliferative activity against human HCT116 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human HCT116 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| HCT-116 | IC50 |
0.31 μM
Compound: 1, MLN-8054
|
Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay
Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay
|
[PMID: 19402633] |
| HCT-116 | IC50 |
0.69 μM
Compound: MLN8054
|
Cytotoxicity against human HCT116 cells after 5 days by MTS assay
Cytotoxicity against human HCT116 cells after 5 days by MTS assay
|
[PMID: 22326168] |
| HCT-116 | IC50 |
0.85 μM
Compound: MLN8054
|
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay
|
[PMID: 30143423] |
| HCT-116 | IC50 |
34 nM
Compound: 4, MLN-8054
|
Inhibition of aurora A autophosphorylation in human HCT116 cells by immunofluorescence method
Inhibition of aurora A autophosphorylation in human HCT116 cells by immunofluorescence method
|
[PMID: 19320489] |
| HCT-116 | IC50 |
34 nM
Compound: 8, MLN8054
|
Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis
Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis
|
[PMID: 26101564] |
| HCT-116 | IC50 |
4 μM
Compound: 4, MLN-8054
|
Inhibition of aurora B in human HCT116 cells assessed as inhibition of histone H3 Ser10 phosphorylation by immunofluorescence method
Inhibition of aurora B in human HCT116 cells assessed as inhibition of histone H3 Ser10 phosphorylation by immunofluorescence method
|
[PMID: 19320489] |
| HCT-116 | IC50 |
5 μM
Compound: 1, MLN-8054
|
Inhibition of Aurora B in human HCT116 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay
Inhibition of Aurora B in human HCT116 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay
|
[PMID: 19402633] |
| HCT-116 | IC50 |
5.2 μM
Compound: 8, MLN8054
|
Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis
Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis
|
[PMID: 26101564] |
| HeLa | IC50 |
0.034 μM
Compound: MLN-8054
|
Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr
Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr
|
[PMID: 17360485] |
| HeLa | IC50 |
5.7 μM
Compound: MLN-8054
|
Inhibition of Aurora B Ser10 phosphorylation in human HeLa cells after 1 hr
Inhibition of Aurora B Ser10 phosphorylation in human HeLa cells after 1 hr
|
[PMID: 17360485] |
| HT-29 | IC50 |
0.15 μM
Compound: 1, MLN-8054
|
Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay
Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay
|
[PMID: 19402633] |
| MCF7 | IC50 |
0.67 μM
Compound: MLN-8054
|
Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| MDA-MB-231 | IC50 |
0.74 μM
Compound: MLN-8054
|
Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| NCI-H460 | IC50 |
0.11 μM
Compound: MLN-8054
|
Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| PC-3 | IC50 |
0.79 μM
Compound: MLN-8054
|
Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| Sf9 | IC50 |
0.004 μM
Compound: MLN-8054
|
Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay
Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay
|
[PMID: 17360485] |
| Sf9 | IC50 |
0.172 μM
Compound: MLN-8054
|
Inhibition of mouse recombinant Aurora B kinase expressed in insect Sf9 cells by radioactive flashplate assay
Inhibition of mouse recombinant Aurora B kinase expressed in insect Sf9 cells by radioactive flashplate assay
|
[PMID: 17360485] |
| Sf9 | IC50 |
172 nM
Compound: MLN8054
|
Inhibition of mouse recombinant Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as substrate and [gamma33P]ATP by flashplate assay
Inhibition of mouse recombinant Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as substrate and [gamma33P]ATP by flashplate assay
|
[PMID: 22803810] |
| Sf9 | IC50 |
172 nM
Compound: MLN8054
|
Inhibition of GST-tagged recombinant mouse Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as peptide substrate by [gamma-33S]ATP binding assay
Inhibition of GST-tagged recombinant mouse Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as peptide substrate by [gamma-33S]ATP binding assay
|
[PMID: 24681066] |
| Sf9 | IC50 |
31 nM
Compound: 8, MLN8054
|
Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP
Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP
|
[PMID: 26101564] |
| Sf9 | IC50 |
4 nM
Compound: MLN8054
|
Inhibition of mouse recombinant Aurora A expressed in Sf9 cells using Biotin-GLRRASLG as substrate and [gamma33P]ATP by flashplate assay
Inhibition of mouse recombinant Aurora A expressed in Sf9 cells using Biotin-GLRRASLG as substrate and [gamma33P]ATP by flashplate assay
|
[PMID: 22803810] |
| Sf9 | IC50 |
4 nM
Compound: MLN8054
|
Inhibition of GST-tagged recombinant mouse Aurora A expressed in Sf9 cells using biotin-GLRRASLG as peptide substrate by [gamma-33S]ATP binding assay
Inhibition of GST-tagged recombinant mouse Aurora A expressed in Sf9 cells using biotin-GLRRASLG as peptide substrate by [gamma-33S]ATP binding assay
|
[PMID: 24681066] |
| Sf9 | IC50 |
4 nM
Compound: MLN8054
|
Inhibition of recombinant mouse Aurora A kinase expressed in Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33]P-ATP by FlashPlate assay
Inhibition of recombinant mouse Aurora A kinase expressed in Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33]P-ATP by FlashPlate assay
|
[PMID: 30502115] |
| SK-OV-3 | IC50 |
0.53 μM
Compound: MLN-8054
|
Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
| SW480 | IC50 |
0.86 μM
Compound: MLN-8054
|
Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA
Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA
|
[PMID: 17360485] |
MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase. MLN8054 is >40-fold more selective for Aurora A compared with the family member Aurora B. MLN8054 selectively inhibits Aurora A over Aurora B in cultured human tumor cells. MLN8054 treatment results in G2/M accumulation and spindle defects and inhibits proliferation in multiple cultured human tumor cells lines. MLN8054 effectively inhibits the growth of cells from diverse tissue origins with IC50 values ranging from 0.11 to 1.43 μM[1]. Treatment of human tumor cells grown in culture with MLN8054 shows a number of morphologic and biochemical changes associated with senescence[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 869363-13-3
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Appearance Solid
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Peso molecular 476.86
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Fòrmula C25H15ClF2N4O2
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Color White to yellow
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SMILES
O=C(C1=CC=C(NC2=NC3=C(CN=C(C4=C3C=CC(Cl)=C4)C5=C(F)C=CC=C5F)C=N2)C=C1)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (10)
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Journal Impact Factor
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Most Recent
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Cancer Res
2017 Sep 15;77(18):4785-4796. PMID: 28720575 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
PLoS Biol
2020 Jun 9;18(6):e3000288. PMID: 32516310 -
EMBO Rep
CK1-mediated phosphorylation of FAM110A promotes its interaction with mitotic spindle and controls chromosomal alignment. [Abstract]2021 Jul 5;22(7):e51847. PMID: 34080749 -
Comput Struct Biotechnol J
Unveiling the Kinomes of Leishmania infantum and L. braziliensis Empowers the Discovery of New Kinase Targets and Antileishmanial Compounds. [Abstract]2019 Feb 8:17:352-361. PMID: 30949306 -
Mol Cell Endocrinol
The N-terminal region of HASPIN regulates phosphorylation of AURKA and meiotic progression in spermatocytes. [Abstract]2025 Aug 28:609:112645. PMID: 40885374 -
Anticancer Drugs
2024 Jan 1;35(1):46-54. PMID: 37449977 -
-
-
J Biomol Screen
Differential determinants of cancer cell insensitivity to antimitotic drugs discriminated by a one-step cell imaging assay. [Abstract]2013 Oct;18(9):1062-71. PMID: 23788527
Solvente y solubilidad
DMSO : 20.83 mg/mL (43.68 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.24 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
MLN8054 is added to human tumor cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 to 0.04 mM. MLN8054 at each dilution is added in triplicate with each replicate on a separate plate. Cells treated with DMSO (n=6 wells per plate; 0.2% final concentration) served as the untreated control. The cells are treated with MLN8054 for 96 h at 37°C in a humidified cell culture chamber. Cell viability in each cell line is measured by using the Cell Proliferation ELISA, BrdU colorimetric kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Nude mice bearing HCT-116 tumors are treated orally once per day for 21 consecutive days with either vehicle control or MLN8054 at doses of 3, 10, or 30 mg/kg. Tumor volumes are measured by using a vernier caliper and calculated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. [Content Brief]
[2]. Huck JJ, et al. MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Mol Cancer Res. 2010 Mar;8(3):373-84. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0971 mL | 10.4853 mL | 20.9705 mL | 52.4263 mL |
| 5 mM | 0.4194 mL | 2.0971 mL | 4.1941 mL | 10.4853 mL | |
| 10 mM | 0.2097 mL | 1.0485 mL | 2.0971 mL | 5.2426 mL | |
| 15 mM | 0.1398 mL | 0.6990 mL | 1.3980 mL | 3.4951 mL | |
| 20 mM | 0.1049 mL | 0.5243 mL | 1.0485 mL | 2.6213 mL | |
| 25 mM | 0.0839 mL | 0.4194 mL | 0.8388 mL | 2.0971 mL | |
| 30 mM | 0.0699 mL | 0.3495 mL | 0.6990 mL | 1.7475 mL | |
| 40 mM | 0.0524 mL | 0.2621 mL | 0.5243 mL | 1.3107 mL |